Neuroactive steroid anaesthetic agents, methods for their preparation and compositions comprising the same are disclosed. Also provided are scaled up and/or GMP methods for preparing neuroactive steroids, such as alfaxalone, alfadolone and alfadolone acetate.

Provided herein is a compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein n, R.sup.19, R.sup.5, R.sup.3a, R.sup.6a, R.sup.6b, R.sup.1, R.sup.2a, R.sup.2b, R.sup.4a, R.sup.4b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.12a, R.sup.12b, R.sup.17b, R.sup.15a, R.sup.15b, R.sup.16a and R.sup.16b are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) and methods of using the compounds, e.g., in the treatment of CNS-related disorders. ##STR00001##

The present invention relates to compounds and methods which may be useful as treatments of diseases.

Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound as shown in formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator of GABA .sub.A receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description. ##STR00001##

Described herein are neuroactive steroids or a pharmaceutically acceptable salt thereof. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. Also provided are pharmaceutical compositions comprising a compound described herein and methods of use and treatment, e.g., such as for inducing sedation and/or anesthesia.

The present application describes process for preparing an ortho-allylated hydroxy aryl compounds such as compounds of Formula (I) by reacting an allylic alcohol with a hydroxy aryl compound in the presence of aluminum compound selected from alumina and aluminum alkoxides and in a non-protic solvent wherein at least one carbon atom ortho to the hydroxy group in the hydroxy aryl compound is unsubstituted. The present application also includes compounds of Formula (I).

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The present invention refers to a new enzymatic process for obtaining 17α-monoesters of cortexolone and/or its 9, 11-dehydroderivatives starting from the corresponding 17α,21-diesters which comprises an enzymatic alcoholysis reaction. Furthermore, the present invention refers to new crystalline forms of cortexolone-17α-propionate and 9,11-dehydro-cortexolone 17α-butanoate.

Disclosed in the present disclosure is a method for preparing 16alpha-hydroxyprednisolone, belonging to the technical field of medicine preparation and processing. In the method, 21-hydroxypregna-1,4,9(11),16-tetraene-3,20-dione-21-acetate is used as a starting material, and subjected to oxidation, bromo-hydroxylation, debromination and alcoholysis, so as to prepare 16alpha-hydroxyprednisolone. The method for preparing 16alpha-hydroxylprednisolone of the present disclosure can effectively control the generation of impurities in the reaction process by improving the disadvantages of traditional processes, and has a mild reaction process and a high overall conversion rate; and the method of the present disclosure has low requirements for a reaction device and low operation costs, is easy to operate, is suitable for industrial production, and has a good market prospect.

Described herein are compositions and methods for hormone replacement therapy that address the shortcomings of the existing methods. Described herein are pharmaceutically effective partial agonistic antiprogestins. The combined application of estrogens (such as estradiol, estriol and conjugated estrogens) and the disclosed partial agonistic antiprogestins can be used in hormone replacement therapy.

Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, wherein Z is a group of the formula (i), (ii), (iii), (iv), or (v), and wherein L.sup.1, L.sup.2, L.sup.3, X.sup.1, X.sup.2, Y, R.sup.z4, R.sup.z5, R.sup.z6, n, R.sup.1, R.sup.2, R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b, R.sup.6a, R.sup.6b, R.sup.7a, R.sup.7b, R.sup.11a, R.sup.11b, R.sup.14, R.sup.17, R.sup.19, R.sup.20, R.sup.23a, R.sup.23b, and R.sup.24 are as defined herein, and pharmaceutical compositions thereof. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of CNS-related conditions in mammals.

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